SU-9516

SKU: orb1225159

Description

A selective CDK2 inhibitor with IC50 of 22 nM; shows less potent for CDK1/CDK4(IC50=40/200 nM), no inhibition on PKC, EGFR, p38MAPK; decreases the phosphorylation of pRb, and increases caspase-3 activation.

Key Properties

• CAS Number: 377090-84-1
• MW: 241.2453
• Purity: >98% (HPLC)
• Formula: C₁₃H₁₁N₃O₂
• SMILES: O=C1NC2=C(C=C(OC)C=C2)/C1=C/C3=CN=CN3
• Target: CDK
• Solubility: 10 mM in DMSO

Bioactivity

• In Vitro:
  SU9516 shows slight activities against PKC, p38, PDGFr and EGFR, with IC50 of >10, >10, 18, and >100 μM. SU9516 (5 μM) decreases cdk2-specific Phosphorylation of pRB and inhibits cell cycle progression in RKO cells. SU9516 (5 μM) also induces apoptosis in RKO and SW480 Cells. SU9516 (5 μM) results in enhanced pRb/E2F complex formation in HT-29 cells. SU9516 enhances presence of E2F species in multiprotein complexes. SU9516 (5 μM) rapidly induces cytochrome crelease, Bax mitochondrial translocation, and apoptosis in association with pronounced down-regulation of the antiapoptotic protein Mcl-1. SU9516 causes down-regulation of Mcl-1 mRNA levels in human leukemia cells. Furthermore, SU9516 treatment results in a marked increase in reactive oxygen species production.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SU9516 | SU 9516

Quick Database Links

Gene Symbol

CDK